Octreotide Acetate Mechanism Of Action For Severe Diarrhea And Flushing Associated With Metastatic Carcinoid Tumors

Sandostatin® LAR Depot (octreotide acetate for injectable suspension) is a somatostatin analogue. Its effects in the body are similar to those of the naturally occurring hormone, except that Sandostatin® LAR Depot remains active much longer than somatostatin.1

Octreotide is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Also, like somatostatin, Sandostatin® LAR Depot suppresses LH response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide.2 By doing so, it can significantly reduce severe diarrhea and flushing that are associated with excess quantities of these bioactive substances.3,4

Sandostatin® LAR Depot’s mechanism of action slows intestinal transport:

  • Rapid gastrointestinal (GI) transit leads to accumulation of fluid in the colon and profuse volumes of watery stool5
  • Sandostatin® (octreotide acetate) slows GI transit and increases fluid absorption by over 300%6

Highlights Of Important Safety Information

Bradycardia, arrhythmia, conduction abnormalities, and other EKG changes may occur. The relationship of these events to octreotide acetate is not established because many of these patients have underlying cardiac disease. Use with caution in at-risk patients.

Sandostatin® LAR Depot (octreotide acetate for injectable suspension) Mechanism of Action

See how Sandostatin® LAR Depot works to suppress the overproduction of certain peptides and amines associated with carcinoid syndrome.

9/13   SDS-1071657

go back to top

Highlights of Important Safety Information

Nutrition: Octreotide may alter absorption of dietary fats. Monitoring of vitamin B12 levels is recommended during therapy with Sandostatin LAR Depot. Patients on total parenteral nutrition (TPN) and octreotide should have periodic monitoring of zinc levels.

Please see below for Important Safety Information.

Getting in Touch Is Easy

Click here to have a Sandostatin® Sales Specialist contact you.

Learn More Now

Real Support

Find out about an information and support program available to your patients. They can get helpful answers from experts and stories of real people coping with carcinoid syndrome.

Learn More About Real Support
 

INDICATIONS AND USAGE:

Sandostatin® LAR Depot (octreotide acetate for injectable suspension) is indicated for patients in whom initial treatment with immediate release Sandostatin® (octreotide acetate) Injection has been shown to be effective and tolerated for:

  • Long-term maintenance therapy in acromegalic patients who have had inadequate response to surgery and/or radiotherapy or for whom surgery and/or radiotherapy is not an option (the goal of treatment in acromegaly is to reduce GH and IGF-1 levels to normal)
  • Long-term treatment of the severe diarrhea and flushing episodes associated with metastatic carcinoid tumors
  • Long-term treatment of the profuse watery diarrhea associated with VIP-secreting tumors

In patients with carcinoid syndrome and VIPomas, the effect of Sandostatin Injection and Sandostatin LAR Depot on tumor size, rate of growth and development of metastases has not been determined.

IMPORTANT SAFETY INFORMATION

Warnings and Precautions:

  • Gallbladder abnormalities may occur: Patients should be monitored periodically.
  • Glucose Metabolism: Hypoglycemia or hyperglycemia may occur. Blood glucose levels should be monitored when Sandostatin LAR Depot treatment is initiated or when the dose is altered. Antidiabetic treatment should be adjusted accordingly.
  • Thyroid Function: Hypothyroidism may occur. Baseline and periodic assessment of thyroid function (TSH, total and/or free T4) is recommended.
  • Cardiac Function: Bradycardia, arrhythmia, conduction abnormalities, and other EKG changes may occur. The relationship of these events to octreotide acetate is not established because many of these patients have underlying cardiac disease. Use with caution in at-risk patients.
  • Nutrition: Octreotide may alter absorption of dietary fats. Monitoring of vitamin B12 levels is recommended during therapy with Sandostatin LAR Depot. Patients on total parenteral nutrition (TPN) and octreotide should have periodic monitoring of zinc levels.

Drug Interactions: The following drugs require monitoring and possible dose adjustment when used with Sandostatin LAR Depot: cyclosporine, insulin, oral hypoglycemic agents, beta-blockers, and bromocriptine. Octreotide has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs. Drugs mainly metabolized by CYP3A4 and which have a low therapeutic index should be used with caution.

Adverse Reactions: The most common adverse reactions occurring in patients receiving Sandostatin LAR Depot are:

  • Acromegaly: biliary abnormalities (52%), diarrhea (36-48%), cholelithiasis (13-38%), abdominal pain or discomfort (11-29%), flatulence (26%), influenza-like symptoms (20%), constipation (19%), headache (15%), anemia (15%), hyperglycemia (15%), injection site pain (2-14%), hypertension (13%), dizziness (12%), fatigue (11%), nausea (10%), vomiting (7%), hypothyroidism (2%), hypoglycemia (2%), and goiter (2%).
  • Carcinoid Tumors and VIPomas: biliary abnormalities (62%), injection site pain (20-50%), nausea (24-41%), abdominal pain (10-35%), fatigue (8-32%), headache (16-30%), hyperglycemia (27%), back pain (8-27%), constipation or vomiting (15-21%), dizziness (18-20%), sinus bradycardia (19%), pruritus (18%), URTI (10-18%), myalgia (4-18%), flatulence (9-16%), arthropathy (8-15%), rash (15%), generalized pain (4-15%), sinusitis (5-12%), conduction abnormalities (9%), hypoglycemia (4%), and arrhythmia (3%).

Please see full Prescribing Information.

References

  1. Battershill PE, Clissold SP. Octreotide: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in conditions associated with excessive peptide secretion. Drugs. 1989;38:658-702.
  2. Sandostatin® LAR Depot [prescribing information]. East Hanover, NJ: Novartis Pharmaceuticals Corp; 2010.
  3. Kaltsas GA, Besser GM, Grossman AB. The diagnosis and medical management of advanced neuroendocrine tumors. Endocr Rev. 2004;25:458-511.
  4. Dueno MI, Bai JC, Santangelo WC, Krejs GJ. Effect of somatostatin analog on water and electrolyte transport and transit time in human small bowel. Dig Dis Sci. 1987;32:1092-1096.
  5. Oberg K. Carcinoid tumors, carcinoid syndrome, and related disorders. In: Larsen PR, Kronenberg HM, Melmed S, Polonsky KS, eds. Williams Textbook of Endocrinology. 10th ed. Philadelphia, PA: W.B. Saunders Company; 2003:1857-1876.
  6. Gregersen T, Gronaek H, Worsoe J, et al. Effects of Sandostatin LAR on gastrointestinal motility in patients with neuroendocrine tumors. Scand J Gastroenterol. 2011;46:895-902.